| 中文名称: | NITD-349 | ||||
|---|---|---|---|---|---|
| 英文名称: | NITD-349 | ||||
| 别名: | N-(4,4-dimethylcyclohexyl)-4,6-difluoro-1H-indole-2-carboxamide;N-(4,4-dimethylcyclohexyl)-4,6-bis(fluoranyl)-1H-indole-2-carboxamide | ||||
| CAS No: | 1473450-62-2 | 分子式: | C17H20F2N2O | 分子量: | 306.35 |
| CAS No: | 1473450-62-2 | ||||
| 分子式: | C17H20F2N2O | ||||
| 分子量: | 306.35 | ||||
包装规格：
1mg 5mg 10mg 50mg 100mg in glass bottle
产品简介：
NITD-349 是 MmpL3 的抑制剂，具有高效的抗分枝杆菌活性，对结合分歧杆菌H37Rv的 MIC50 值为23 nM。
溶解性：
溶于DMSO （ ≥310 mg/mL）
储备液保存：
-80°C, 2 years
-20°C, 1 year
-20°C, 1 year
靶点：
MIC50: 23 nM (Mycobacterium tuberculosis H37Rv)
体外研究：
NITD-349 shows bactericidal activity against in vitro replicating Mycobacterium tuberculosis (Mtb) and also are active against intramacrophage Mtb. Kill kinetic analysis of these compounds showed both concentration- and time-dependent killing of Mtb cells with 3- to 4-log colony-forming unit (CFU) reductionwithin 3 days of treatment. The cidal activity profile of NITD-304 is similar to that of isoniazid for which rapid killing is noticed at concentrations greater than 0.2 μM. The MIC activity of NITD349 against various MDR Mtb strains ranges from 0.04 to 0.08 μM. NITD-349 shows high permeability and moderate in vitro metabolic clearance in mouse and human hepatic microsomes.
体内研究：
In the acute murine efficacy modelNITD-349 shows favorable oral pharmacokinetic (PK) properties in rodents and dogs and are efficacious in mouse models of both acute and chronic Mycobacterium tuberculosis infection. In the acute murine efficacy model, treatment of mice with NITD-349 at doses of 12.5 and 50 mg/kg resulted in 0.9- and 3.4-log CFU reduction in lung tissue. In an established infection mouse model, after 2 weeks of treatment, the efficacy of NITD-349 is comparable to the first-line TB drug rifampicin and is better than ethambutol. Four weeks of treatment at 100 mg/kg with NITD-349 results in 2.38-log CFU reductions.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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安全说明：
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参考文献 & 客户发表文献
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稀释公式
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